AR088801A1 - Compuestos inhibidores de la fosfodiesterasa del tipo 10a - Google Patents

Compuestos inhibidores de la fosfodiesterasa del tipo 10a

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AR088801A1
AR088801A1 ARP120104208A ARP120104208A AR088801A1 AR 088801 A1 AR088801 A1 AR 088801A1 AR P120104208 A ARP120104208 A AR P120104208A AR P120104208 A ARP120104208 A AR P120104208A AR 088801 A1 AR088801 A1 AR 088801A1
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alkoxy
alkyl
members
group
hydrogen
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Behl Berthold
Ochse Michael
Dinges Jrgen
Jakob Clarissa
A Black Lawrence
Drescher Karla
Geneste Herve
turner Sean
Laplanche Loic
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Abbott Gmbh & Co Kg
Abbvie Inc
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Application filed by Abbott Gmbh & Co Kg, Abbvie Inc filed Critical Abbott Gmbh & Co Kg
Publication of AR088801A1 publication Critical patent/AR088801A1/es

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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D401/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) donde Q es O ó S; X¹ es N o CH; X² es N o C-R⁷; X³ es O, S, -X⁴=C(R⁸)-, donde C(R⁸) está unido al átomo de carbono que se une a R² o -X⁵=C(R⁹)-, donde X⁵ está unido al átomo de carbono que se une a R²; X⁴ es N o C-R⁹; X⁵ es N; Het se selecciona entre i) hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que no está sustituido o puede tener 1, 2, 3 ó 4 sustituyentes idénticos o diferentes Rˣ, ii) hetarilo bicíclico fusionado con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, benzotienilo o benzofurilo, donde hetarilo bicíclico, benzotienilo y benzofurilo, en forma independiente entre sí, no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes idénticos o diferentes Rˣ, y iii) fenilo, que se une a un radical hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que además de hetarilo monocíclico, puede tener 1, 2 ó 3 sustituyentes idénticos o diferentes Rˣ, donde Rˣ se selecciona entre el grupo que consiste en H, halógeno, alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄-alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, OH, hidroxi-alquilo C₁₋₄, O-cicloalquilo C₃₋₆, benciloxi, C(O)O-(alquilo C₁₋₄), O-(alquil C₁₋₄)-CO₂H, N(Rˣ¹)(Rˣ²), C(O)N(Rˣ¹)(Rˣ²), alquil C₁₋₄-N(Rˣ¹)(Rˣ²), -NRˣ³-C(O)-N(Rˣ¹)(Rˣ²), NRˣ³-C(O)O-(alquilo C₁₋₄), -N(Rˣ³)-SO₂-Rˣ⁴, fenilo, CN, -SF₅, -OSF₅, -SO₂Rˣ⁴, -SRˣ⁴ y trimetilsililo, donde Rˣ¹, Rˣ², Rˣ³ y Rˣ⁴, en forma independiente entre sí se seleccionan entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, fluoroalquilo C₁₋₄ y cicloalquilo C₃₋₆ o Rˣ¹ y Rˣ² forman junto con el átomo de N al cual están unidos un heterociclo con nitrógeno de entre 3 y 7 miembros que puede tener 1, 2 ó 3 heteroátomos o grupos que contienen heteroátomos adicionales diferentes o idénticos seleccionados entre el grupo de O, N, S, SO y SO₂ como miembros del anillo y que puede tener 1, 2, 3, 4, 5 ó 6 sustituyentes seleccionados entre alquilo C₁₋₄; o dos radicales Rˣ que se unen a átomos de carbono adyacentes pueden formar un radical carbocíclico fusionado saturado de 5 ó 6 miembros o un radical heterocíclico fusionado de 5 ó 6 miembros con 1, 2 ó 3 heteroátomos como miembros del anillo, que se seleccionan entre O, S y N; R¹ se selecciona entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alquilsulfanilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alquilsulfanil C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ², NRˣ¹Rˣ²-alcoxi C₁₋₄ y la porción Y¹-Cyc¹; R² se selecciona entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN y NRˣ¹Rˣ²; A representa uno de los restos de fórmula (A¹), (A²), (A³), (A⁴) ó (A⁵) donde * indica el punto de unión a Het y al átomo de nitrógeno, respectivamente; R³, R⁴, R⁵, R⁶ en forma independiente entre sí se seleccionan entre el grupo que consiste en hidrógeno, halógeno, alquilo C₁₋₄, trimetilsililo, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, o los radicales junto con los átomos de carbono a los cuales están unidos forman un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo o los radicales R³, R⁴ o los radicales R⁵, R⁶ junto con el átomo de carbono a los cuales están unidos forman un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo; A es un O, NR³ᵃ, CR³ᵇR³ᶜ o alcandiilo C₂₋₃ lineal, donde una de las porciones CH₂ de alcandiilo C₂₋₃ puede reemplazarse por oxígeno o NR³ᵃ, y donde 1, 2, 3, ó 4 de los átomos de hidrógeno de alcandiilo C₂₋₃ puede reemplazarse por un radical R³ᵈ, donde R³ᵃ es hidrógeno o alquilo C₁₋₄, R³ᵇ, R³ᶜ en forma independiente entre sí se seleccionan entre el grupo que consiste en hidrógeno, halógeno, alquilo C₁₋₄ o R³ᵇ y R³ᶜ juntos forman alcandiilo C₂₋₃; R³ᵈ se selecciona entre el grupo que consiste en halógeno y alquilo C₁₋₄; R³ᵉ, R³ᶠ en forma independiente entre sí se seleccionan entre el grupo que consiste en hidrógeno y alquilo C₁₋₄; R⁷ se selecciona entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alquilsulfanilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alquilsulfanil C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ², NRˣ¹Rˣ²-alcoxi C₁₋₄ y la porción Y²-Cyc²; R⁸ se selecciona entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN y NRˣ¹Rˣ²; R⁹ se selecciona entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alquilsulfanilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alquilsulfanil C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ², NRˣ¹Rˣ²-alcoxi C₁₋₄ y la porción Y³-Cyc³; Y¹, Y², Y³ en forma independiente entre sí se seleccionan entre un enlace químico, CH₂, O, O-CH₂, NRʸ, NRʸ-CH₂, NRʸ-S(O)₂, S, S(O), S(O)₂, 1,2-etandiilo, 1,2-etendiilo o 1,2-etindiilo, donde Rʸ se selecciona entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, alquil C₁₋₄carbonilo, alquil C₁₋₄sulfonilo, fluoroalquil C₁₋₄sulfonilo; Cyc¹, Cyc², Cyc³ en forma independiente entre sí se seleccionan entre el grupo que consiste en fenilo, naftilo, radicales heteromonocíclicos saturados o parcialmente insaturados de entre 4 y 8 miembros, radicales heterobicíclicos saturados o parcialmente insaturados de entre 7 y 10 miembros, hetarilo monocíclico de 5 ó 6 miembros, y hetarilo bicíclico de entre 8 y 10 miembros, donde los radicales heteromonocíclicos y heterobicíclicos saturados o parcialmente insaturados tienen 1, 2, 3 ó 4 heteroátomos o grupos que contienen heteroátomos como miembros del anillo, que se seleccionan entre O, S, SO, SO₂ y N, y donde el hetarilo monocíclico de 5 ó 6 miembros y el hetarilo bicíclico de entre 8 y 10 miembros tiene 1, 2, 3 ó 4 heteroátomos como miembros del anillo, que se seleccionan entre O, S y N, donde fenilo, naftilo, los radicales heteromonocíclicos y heterobicíclicos satu
ARP120104208A 2011-11-09 2012-11-08 Compuestos inhibidores de la fosfodiesterasa del tipo 10a AR088801A1 (es)

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